Uses for Riluzole

Amyotrophic Lateral Sclerosis

Has been shown to slow disease progression and prolong survival to a modest degree (e.g., by about 2–3 months); because of this possible benefit, experts recommend that the drug should be offered to patients with ALS.124273435

Riluzole Dosage and Administration

General

Measure serum aminotransferases, including ALT levels, before and during riluzole therapy.1 (See Hepatic Effects under Cautions.)

Administration

Oral Administration

Dosage

Adults

Amyotrophic Lateral Sclerosis

Oral

Special Populations

Hepatic Impairment

No specific dosage recommendations; however, use not recommended in patients with aminotransferase concentrations >5 times ULN or evidence of liver dysfunction.1 (See Hepatic Impairment under Cautions.)

Contraindications

Warnings/Precautions

Sensitivity Reactions

Hypersensitivity Reactions

Hepatic Effects

Liver injury, including fatalities, reported.1 Asymptomatic elevations of aminotransferase concentrations (e.g., ALT) also reported and have recurred following rechallenge with the drug.1 Maximum increases in ALT occurred within the first 3 months of therapy.1

Monitor serum aminotransferase concentrations prior to and during therapy;1 also monitor for signs and symptoms of hepatic injury (monthly for the first 3 months of treatment, then periodically thereafter).1 Use not recommended in patients with aminotransferase concentrations >5 times ULN.1 Discontinue therapy if there is evidence of liver dysfunction (e.g., elevated bilirubin concentrations).1

Elimination Route

Half-life

Stability

Storage

Oral

Tablets

Actions and Spectrum

Precise mechanism of action has not been fully elucidated1 but appears to involve interference with the effects mediated by excitatory amino acids (EAAs) in the CNS, possibly through inhibition of glutamic acid release,234569111215171827 blockade or inactivation of voltage-dependent sodium channels,45671517181927 and/or activation of a G-protein-dependent signal transduction pathway.61727

May act via noncompetitive blockade of EAA receptors;514 however, does not appear to bind to any known glutamate receptor.246

Exhibits neuroprotective properties in vitro and in vivo in animals, including inhibition of neuronal toxicity associated with exposure to EAAs 7 or cerebrospinal fluid from ALS patients,67 and inhibits neuronal toxicity associated with anoxia479 or focal or global ischemia.234679

Prolonged survival in a study in a transgenic mouse model of ALS but did not delay onset of the disease.2122

Advice to Patients

Importance of patients informing clinician of any manifestations of possible liver injury (e.g., yellowing of the whites of the eyes).1

35. . Practice advisory on the treatment of amyotrophic lateral sclerosis with riluzole: report of the Quality Standards Subcommittee of the American Academy of Neurology. Neurology. 1997; 49:657-9. http://www.ncbi.nlm.nih.gov/pubmed/9305318?dopt=AbstractPlus